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50 results
  • Cardiac Arrest Due to Benzonatate Overdose. [Journal Article]
    Am J Case Rep 2019; 20:640-642Jin C, Zahid E, … Bedi P
  • CONCLUSIONS: Ingestion of benzonatate, a widely prescribed antitussive, may pose a risk to patients due to the potential for rapid development of life-threatening adverse events and limited treatment options in the overdose setting, not only in children but also in adults. Rational prescribing and patient education are needed.
  • The Antitussive Benzonatate Is Not Tumorigenic in Rodent Carcinogenicity Studies. [Journal Article]
    Toxicol Pathol 2018; 46(6):683-692Teo S, Paranjpe M, … Brown T
  • Benzonatate is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Rodent carcinogenicity studies were performed in Tg.rasH2 mice and Wistar Han rats. Mice were orally gavaged benzonatate at 10, 30, 75, and 100 mg/kg/day for males and 5, 15, and 50 mg/kg/day for females. Rats were gavaged at 10, 30, and 90 mg/kg/day for males and 5, 15, and 50 mg/kg/day for females…
  • Genotoxicity assessment of the novel antitussive agent Benzonatate and its major metabolite. [Journal Article]
    Mutat Res Genet Toxicol Environ Mutagen 2018 May - Jun; 829-830:19-25Teo S, Madraymootoo W, … McKeon M
  • Benzonatate (TESSALON®) is a peripherally acting oral antitussive. It undergoes rapid ester hydrolysis producing 4-(butylamino) benzoic acid (BBA) and methylated polyethylene glycol (MPG) metabolites, which are eliminated in urine and feces. The nonclinical and clinical efficacy of Benzonatate has been demonstrated over the last 60 years, but its safety was not fully assessed. In this study, we t…
  • Discovery of Novel Human Epidermal Growth Factor Receptor-2 Inhibitors by Structure-based Virtual Screening. [Journal Article]
    Pharmacogn Mag 2016 Apr-Jun; 12(46):139-44Shi Z, Yu T, … Liu R
  • CONCLUSIONS: Together, our findings may provide successful application of virtual screening studies in the lead discovery process, and suggest that our discovered small molecules could be effective HER2 inhibitor candidates for further study.A series of elegant bioinformatics approaches, including virtual screening and molecular dynamics (MD) simulations were took advantage to identify human epidermal growth factor receptor-2 (HER2) inhibitors. Molecular docking recognized top 10 candidate compounds, which showed spectrum affinity to HER2. Further, MD simulations suggested that ZINC08214629 (Nonoxynol-9) and ZINC03830276 (Benzonatate) in candidate compounds were identified as potential "new use" drugs against HER2-targeted anti-breast cancer therapeutics. Abbreviations used: HER2: Human epidermal growth factor receptor-2, FDA: Food and Drug Administration, PDB: Protein Database Bank, RMSDs: Root mean square deviations, SPC: Single point charge, PME: Particle mesh Ewald, NVT: Constant volume, NPT: Constant pressure, RMSF: Root-mean-square fluctuation.
  • Benzonatate inhibition of voltage-gated sodium currents. [Journal Article]
    Neuropharmacology 2016; 101:179-87Evans MS, Maglinger GB, … Johnson SR
  • Benzonatate was FDA-approved in 1958 as an antitussive. Its mechanism of action is thought to be anesthesia of vagal sensory nerve fibers that mediate cough. Vagal sensory neurons highly express the Nav1.7 subtype of voltage-gated sodium channels, and inhibition of this channel inhibits the cough reflex. Local anesthetics inhibit voltage-gated sodium channels, but there are no reports of whether …
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